| 中文名称: | N-type calcium channel blocker-1 | ||||
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| 英文名称: | N-type calcium channel blocker-1 | ||||
| 别名: | N-type calcium channel blocker-1 N-type calcium channel blocker-1 | ||||
| CAS No: | 241499-17-2 | 分子式: | C31H47N3 | 分子量: | 461.73 |
| CAS No: | 241499-17-2 | ||||
| 分子式: | C31H47N3 | ||||
| 分子量: | 461.73 | ||||
基本信息
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产品编号： |
N11025 |
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产品名称： |
N-type calcium channel blocker-1 |
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CAS: |
241499-17-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
461.73 |
-20℃ |
1个月 |
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化学名： |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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生物活性
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产品描述 |
一种有口服活性的麻醉剂，可阻断N型钙离子通道(N-typecalciumchannels)。 |
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靶点 |
IC50:0.7μM (N-type calcium channels) |
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体外研究 |
N-type calcium channel blocker-1 shows good activities in the IMR32 assay (IC50=0.7μM).N-type calcium channel blocker-1 is the most orally active N-type calcium channel blocker for analgesia found in a series of compounds. |
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体内研究 |
N-type calcium channel blocker-1 shows good activities in the acetic acid anti-writhing model (ED50=4mg/kg,iv). N-type calcium channel blocker-1 exhibits oral activity (ED50=12mg/kg,po).A time course study of N-type calcium channel blocker1 in the anti-writhing model indicates that the CF-1 mice have maximal effect at 120 min after oral dosing at 60mg/kg.Further evaluation of N-type calcium channel blocker-1 demonstrates several important and advantageous features:the pharmacokinetic profile of N-type calcium channel blocker-1 is improved (Versus of 5.9L/kg and CL of 26mL/min/kg) and the logPn of 26 is favorable for CNS agent (logPn measured to be 3.20). |
推荐实验方法(仅供参考)
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激酶实验： |
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N-type calcium channel blocker-1 is dissolved and diluted in DMSO.Different concentrations of the test compounds (N-type calcium channel blocker-1,et al.) are added to assay buffer containing approximately 3×106 loaded cells with 5mM nitrendipine added to block l-type calcium channels. Samples are incubated for 10 min for then emission signals at 400 and 490nm are acquired from each cuvette at 30℃ for 50s.At 20s after the start of reading,cells are depolarized by the addition of a high K+ solution.Drug effects are expressed as a percentage of the amplitude of the K+- evoked change in intracellular calcium in drug treated compared to control experiments.PD-15130714 is run in parallel as a standard in each assay to compare the relative potencies determined.IC50 values of test compounds are calculated by fitting a fourparameter logistic function to the data using the least squares method. |
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动物实验: |
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Rats Three Wistar rats receive a 5mg/kg bolus intravenous dose of each compound (N-type calcium channel blocker-1,et al.) as a solution and serial plasma samples are collected at various times up to 24hr postdose.Plasma samples are analyzed using direct protein precipitation with acetonitrile and the compound is quantitated by SciexLC/MS/MS system.A Betasil phenyl column (2.1 mm 12 cm) is used with a mobile phase of acetonitrile:0.1% acetic acid (70:30,v/v). Mice Male,CF-1 mice (26 and 30g) are given a single,intraperitoneal injection of 0.6% acetic acid.This injection evoked abdominal constrictions,defined as discrete episodes of torso and hind limb stretching with or without neck arching,are counted and recorded for 5 min,beginning 7 min after acetic acid injection.The mice are individually housed in Nalgene cages and allowed to move freely during the experimental period (12 min).Animals are sacrificed by CO2 asphyxiation immediately after the 5-min observation period.Test compounds (N-type calcium channel blocker-1,et al.) are administered by intravenous or oral routes approximately 10 min prior to administering the acetic acid.The dose response relationship for antinociceptive effects during the acetic acid writhing test are assessed by plotting the incidence of abdominal constrictions against dose of the test compound.ED50 values are calculated using a four parameter logistic function. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
